Benzarone is given by mouth and applied topically for treatment
of various vascular peripheral disorders.The decision to suspend the marketing
authorization results from several reports of toxic hepatitis, including one fatal
case from within Germany. The product remains registered in Italy and France.
생물학적 활성
Benzarone is an active metabolite of the urate anion transporter 1 (URAT1) inhibitor benzbromarone. It inhibits URAT1 in Xenopus oocytes expressing the human enzyme (IC50 = 2.8 μM). Benzarone also inhibits the tyrosine phosphatase activity of eyes absent homolog 3 (EYA3; IC50 = 17.5 μM), as well as reduces the proliferation and migration of human umbilical vein endothelial cells (HUVECs) when used at a concentration of 7.5 μM. It uncouples oxidative phosphorylation in isolated rat liver mitochondria and induces apoptosis and necrosis in isolated rat hepatocytes. Benzarone (25 μg/g) reduces tumor growth in an A-673 Ewing sarcoma mouse xenograft model.
Safety Profile
Poison by
intraperitoneal route. An experimental
teratogen. Other experimental reproductive
effects. A flammable liquid. When heated to
decomposition it emits acrid and irritating
smoke and fumes. See also KETONES.
